Erlotinib

Summary

Erlotinib (CHEMBL553) is an approved small-molecule antineoplastic agent (ATC L01EB02) targeting SLCO2B1 and EGFR; indicated across 68 conditions including neoplasm and head and neck squamous cell carcinoma; with CIViC clinical evidence for 209 variant-indication associations (e.g. EGFR L858R in lung non-small cell carcinoma).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EB02
• Targets: 2 (SLCO2B1, EGFR)
• Indications: 68 conditions
• Clinical trials: 496
• Precision-oncology evidence (CIViC): 209 variant–indication associations
• Chemistry: 393.4 Da · C22H23N3O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL553
Name	Erlotinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	176870
ChEBI	CHEBI:114785
ATC	L01EB02
Molecular formula	C22H23N3O4
Molecular weight	393.4
InChIKey	AAKJLRGGTJKAMG-UHFFFAOYSA-N

SMILES: COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC

IUPAC name: N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine

ChEBI definition: A quinazoline compound having a (3-ethynylphenyl)amino group at the 4-position and two 2-methoxyethoxy groups at the 6- and 7-positions.

Pharmacological roles (ChEBI): antineoplastic agent, protein kinase inhibitor, epidermal growth factor receptor antagonist.

Also known as: CP-358,774, CP-358774, CP-35877401, Erlotinib, R-1415, RG-1415, Ro-508231, Tarceva, erlotinib, SID26757996, SID85267493, SID103905339

Parent form; salt/anhydrous children: CHEMBL1079742, CHEMBL5220042

Patent coverage: 27,961 distinct patent families (108,300 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 105,781 (98%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
SLCO2B1	OATP2B1	Inhibition	6.28	0%	O94956
EGFR	epidermal growth factor receptor	Inhibition	7.04	17.5%	P00533

Broader ChEMBL bioactivity targets: 134 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Homeodomain-interacting protein kinase 4, Serine/threonine-protein kinase SBK1, Prelamin-A/C, Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, Solute carrier organic anion transporter family member 2B1, Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Mitotic checkpoint serine/threonine-protein kinase BUB1, Receptor tyrosine-protein kinase erbB-2.

Bioactivity

ChEMBL activities: 559 potent at pChembl ≥ 5 of 585 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
EGFR	10.54	IC50	0.03	nM	CHEMBL_ACT_25098074
EGFR	10.23	IC50	0.06	nM	CHEMBL_ACT_25098090
EGFR	10	Ki	0.1	nM	CHEMBL_ACT_15135570
EGFR	10	Ki	0.1	nM	CHEMBL_ACT_15135690
EGFR	10	Ki	0.1	nM	CHEMBL_ACT_16452429
EGFR	10	Ki	0.1	nM	CHEMBL_ACT_16452431
EGFR	10	Ki	0.1	nM	CHEMBL_ACT_16513263
EGFR	10	IC50	0.1	nM	CHEMBL_ACT_3261320
EGFR	9.96	IC50	0.11	nM	CHEMBL_ACT_26153964
EGFR	9.7	IC50	0.2	nM	CHEMBL_ACT_3261330
EGFR	9.52	Ki	0.3	nM	CHEMBL_ACT_15135691
EGFR	9.52	Ki	0.3	nM	CHEMBL_ACT_16452430
EGFR	9.46	Kd	0.35	nM	CHEMBL_ACT_2898898
EGFR	9.46	Kd	0.35	nM	CHEMBL_ACT_7575327
EGFR	9.4	IC50	0.4	nM	CHEMBL_ACT_16739489
EGFR	9.4	IC50	0.4	nM	CHEMBL_ACT_2206757
EGFR	9.4	IC50	0.4	nM	CHEMBL_ACT_22835793
EGFR	9.4	IC50	0.4	nM	CHEMBL_ACT_25535994
EGFR	9.33	Kd	0.47	nM	CHEMBL_ACT_2898860
EGFR	9.33	Kd	0.47	nM	CHEMBL_ACT_7575326
EGFR	9.32	Kd	0.48	nM	CHEMBL_ACT_2898708
EGFR	9.32	Kd	0.48	nM	CHEMBL_ACT_7575322
EGFR	9.3	IC50	0.5	nM	CHEMBL_ACT_16410660
EGFR	9.28	Kd	0.52	nM	CHEMBL_ACT_2898784
EGFR	9.28	Kd	0.52	nM	CHEMBL_ACT_2898822
EGFR	9.28	Kd	0.52	nM	CHEMBL_ACT_7575324
EGFR	9.28	Kd	0.52	nM	CHEMBL_ACT_7575325
EGFR	9.25	IC50	0.56	nM	CHEMBL_ACT_26239127
EGFR	9.22	IC50	0.6	nM	CHEMBL_ACT_1682080
EGFR	9.22	IC50	0.6	nM	CHEMBL_ACT_20657368

Target pathways

Aggregated over 2 target gene(s): SLCO2B1, EGFR.

Top Reactome pathways

44 total, by targets touching each:

Pathway	Targets	Genes
Signaling by ERBB2	1	EGFR
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants	1	EGFR
Signaling by ERBB4	1	EGFR
SHC1 events in ERBB2 signaling	1	EGFR
PLCG1 events in ERBB2 signaling	1	EGFR
PIP3 activates AKT signaling	1	EGFR
Signaling by EGFR	1	EGFR
GRB2 events in EGFR signaling	1	EGFR
GAB1 signalosome	1	EGFR
SHC1 events in EGFR signaling	1	EGFR
EGFR downregulation	1	EGFR
Heme degradation	1	SLCO2B1
GRB2 events in ERBB2 signaling	1	EGFR
PI3K events in ERBB2 signaling	1	EGFR
EGFR interacts with phospholipase C-gamma	1	EGFR
EGFR Transactivation by Gastrin	1	EGFR
Constitutive Signaling by Aberrant PI3K in Cancer	1	EGFR
Transport of small molecules	1	SLCO2B1
Transport of vitamins, nucleosides, and related molecules	1	SLCO2B1
SLC-mediated transmembrane transport	1	SLCO2B1
Signal transduction by L1	1	EGFR
Constitutive Signaling by EGFRvIII	1	EGFR
Inhibition of Signaling by Overexpressed EGFR	1	EGFR
RAF/MAP kinase cascade	1	EGFR
ERBB2 Regulates Cell Motility	1	EGFR
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	1	EGFR
Organic anion transport by SLCO transporters	1	SLCO2B1
ERBB2 Activates PTK6 Signaling	1	EGFR
Cargo recognition for clathrin-mediated endocytosis	1	EGFR
Clathrin-mediated endocytosis	1	EGFR

Dominant GO biological processes

GO term	Targets
xenobiotic metabolic process	1
monoatomic ion transport	1
obsolete organic anion transport	1
bile acid and bile salt transport	1
heme catabolic process	1
sodium-independent organic anion transport	1
transmembrane transport	1
transport across blood-brain barrier	1
prostaglandin transport	1
cell morphogenesis	1
ossification	1
embryonic placenta development	1
positive regulation of protein phosphorylation	1
hair follicle development	1
ubiquitin-dependent protein catabolic process	1

Indications & clinical

Indications

68 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
neoplasm	3	MONDO:0005070	EFO:0000616
head and neck squamous cell carcinoma	3	MONDO:0010150	EFO:0000181
exocrine pancreatic carcinoma	3	MONDO:0005192	EFO:0002618
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
squamous cell carcinoma	3	MONDO:0005096	EFO:0000707
oral cavity neoplasm	3	MONDO:0021245	EFO:0003868
hepatocellular carcinoma	3	MONDO:0007256	EFO:0000182
lung large cell carcinoma	3	MONDO:0003050	EFO:0003050
pancreatic neoplasm	3	MONDO:0021040	EFO:0003860
head and neck cancer	3	MONDO:0005627	EFO:0006859
lung neoplasm	3	MONDO:0021117	MONDO:0008903
malignant pancreatic neoplasm	3	MONDO:0009831	EFO:1000359
colorectal neoplasm	3	MONDO:0005335	MONDO:0005575
leukemia	2	MONDO:0005059	EFO:0000565
psoriasis	2	MONDO:0005083	EFO:0000676
ependymoma	2	MONDO:0016698	EFO:1000028
myelodysplastic syndrome	2	MONDO:0018881	EFO:0000198
acquired polycythemia vera	2	MONDO:0009891	EFO:0002429
carcinoma	2	MONDO:0004993	EFO:0000313
acute myeloid leukemia	2	MONDO:0018874	EFO:0000222
minimally invasive lung adenocarcinoma	2	MONDO:0004991	EFO:0000308
germ cell tumor	2	MONDO:0005040	EFO:0000514
glioblastoma	2	MONDO:0018177	EFO:0000519
mesothelioma	2	MONDO:0005065	EFO:0000588
carcinoma of esophagus	2	MONDO:0019086	EFO:0002916
ovarian neoplasm	2	MONDO:0021068	EFO:0003893
nasopharyngeal neoplasm	2	MONDO:0005375	EFO:0004252
thymoma	2	MONDO:0006456	EFO:1000581
gliosarcoma	2	MONDO:0016681	EFO:1001465
diffuse intrinsic pontine glioma	2	MONDO:0006033	EFO:1000026
neuroendocrine neoplasm	2	MONDO:0019496	EFO:1001901
fallopian tube neoplasm	2	MONDO:0021092	MONDO:0002158
skin neoplasm	2	MONDO:0002531	MONDO:0002898
breast neoplasm	2	MONDO:0021100	MONDO:0007254
ovarian cancer	2	MONDO:0008170	MONDO:0008170
hematopoietic and lymphoid system neoplasm	2	MONDO:0002334	MONDO:0044881
chronic hepatitis C virus infection	1	MONDO:0005354	EFO:0004220
clear cell renal carcinoma	1	MONDO:0005005	EFO:0000349
renal cell carcinoma	1	MONDO:0005086	EFO:0000681
anaplastic astrocytoma	1	MONDO:0016684	EFO:0002499
anaplastic oligodendroglioma	1	MONDO:0016696	EFO:0002501
Ebola hemorrhagic fever	1	MONDO:0005737	EFO:0007243
rectal cancer	1	MONDO:0006519	EFO:1000657
lung adenocarcinoma	1	MONDO:0005061	EFO:0000571
melanoma	1	MONDO:0005105	EFO:0000756
plasma cell myeloma	1	MONDO:0009693	EFO:0001378
central nervous system neoplasm	1	MONDO:0006130	EFO:1000158
brain cancer	1	MONDO:0001657	MONDO:0001657
glioma	1	MONDO:0021042	MONDO:0003268
astrocytoma (excluding glioblastoma)	1	MONDO:0019781	MONDO:0016691
colonic neoplasm	1	MONDO:0005401	EFO:0004288
pharynx cancer	0	MONDO:0005517	EFO:0005577

16 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 496.

Phase distribution

Phase	Trials
PHASE2	247
PHASE1	99
PHASE3	58
PHASE1/PHASE2	48
Not specified	24
PHASE4	14
PHASE2/PHASE3	4
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00642733	PHASE4	TERMINATED	A Study of First Line Treatment With Tarceva (Erlotinib) in Combination With Gemcitabine in Patients With Locally Advanced Unresectable or Metastatic Pancreatic Cancer
NCT00949910	PHASE4	COMPLETED	An Expanded Access Program of Tarceva (Erlotinib) in Participants With Advanced Non-Small Cell Lung Cancer (NSCLC)
NCT01066884	PHASE4	COMPLETED	A Study of First or Second Line Treatment With Tarceva (Erlotinib) in Patients With Advanced Non-Small Cell Lung Cancer
NCT01196078	PHASE4	COMPLETED	A Study of Tarceva (Erlotinib) in Elderly Patients With Advanced Non-Small Cell Lung Cancer
NCT01230710	PHASE4	COMPLETED	A Study of Tarceva (Erlotinib) in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer Following 4 Cycles of Platinum-based Chemotherapy Without Disease Progression
NCT01287754	PHASE4	COMPLETED	A Study of Tarceva (Erlotinib) in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer Who Present EGFR Mutations
NCT01320501	PHASE4	SUSPENDED	Experience of Erlotinib in Patients With Advanced Non-Small Cell Lung Cancer
NCT01402089	PHASE4	COMPLETED	Cytochrom p450 3A4 and 1A2 Phenotyping for the Individualization of Treatment With Sunitinib or Erlotinib in Cancer Patients
NCT01609543	PHASE4	COMPLETED	A Study of Tarceva (Erlotinib) in First Line in Patients With Locally Advanced or Metastatic Lung Adenocarcinoma With EGFR Mutations
NCT02000531	PHASE4	COMPLETED	Progression Free Survival (PFS) Using Erlotinib for Non-Small-Cell Lung Cancer (NSCLC) in Chinese Population
NCT02031601	PHASE4	UNKNOWN	Intercalated Combination of Chemotherapy and Tyrosine Kinase Inhibitors as First-line Treatment for Patients With Non-Small-Cell Lung Cancer
NCT02399566	PHASE4	UNKNOWN	Clinical Trial of Erlotinib and Pemetrexed for Maintenance Treatment in Lung Adenocarcinoma
NCT03460678	PHASE4	TERMINATED	Randomized Comparative Study of Erlotinib and Pemetrexed in the Maintenance Treatment of Advanced Lung Cancer Patients.
NCT04145570	PHASE4	COMPLETED	A Single-Dose,ComparativeBioavailability Study ofTwo Formulations ofErlotinib150mgTabletsunderFastingConditions
NCT02152631	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Abemaciclib (LY2835219) in Participants With Previously Treated KRAS Mutated Lung Cancer
NCT02411448	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Ramucirumab (LY3009806) in Combination With Erlotinib in Previously Untreated Participants With EGFR Mutation-Positive Metastatic NSCLC (RELAY)
NCT00153803	PHASE3	COMPLETED	Erlotinib or Placebo Following Chemoradiotherapy (Chemo/RT) in Stage III Non-Small Cell Lung Cancer (NSCLC)
NCT00265824	PHASE3	COMPLETED	Optimized Chemotherapy Followed by Maintenance With Bevacizumab With or Without Erlotinib in Treating Patients With Metastatic Colorectal Cancer That Cannot be Removed by Surgery (DREAM)
NCT00268684	PHASE3	UNKNOWN	Comparison Study of WBRT and SRS Alone Versus With Temozolomide or Erlotinib in Patients With Brain Metastases of NSCLC
NCT00300586	PHASE3	COMPLETED	IFCT-GFPC 05.02 A Randomized Phase III Trial Assessing in Patients With Advanced Non-small Cell Lung Cancer
NCT00349219	PHASE3	COMPLETED	TORCH: A Study of Tarceva or Chemotherapy for the Treatment of Advanced Non Small Cell Lung Cancer
NCT00364351	PHASE3	COMPLETED	Efficacy Trial Comparing ZD6474 With Erlotinib in NSCLC After Failure of at Least One Prior Chemotherapy
NCT00373425	PHASE3	COMPLETED	A Study of Erlotinib (Tarceva) After Surgery With or Without Adjuvant Chemotherapy in Non-Small Cell Lung Carcinoma (NSCLC) Patients Who Have Epidermal Growth Factor Receptor (EGFR) Positive Tumors
NCT00402779	PHASE3	COMPLETED	Erlotinib Prevention of Oral Cancer (EPOC)
NCT00412217	PHASE3	TERMINATED	A Study of Erlotinib (Tarceva) in Participants With Resected Head and Neck Squamous Cell Cancer
NCT00440167	PHASE3	UNKNOWN	Capecitabine/Erlotinib Followed of Gemcitabine Versus Gemcitabine/Erlotinib Followed of Capecitabine
NCT00440414	PHASE3	COMPLETED	Trial of Pemetrexed Versus Erlotinib in Pretreated Patients With Non Small Cell Lung Cancer (NSCLC)
NCT00442455	PHASE3	COMPLETED	Erlotinib,Radiation and Cisplatin in Patients With Complete Resected Squamous Cell Carcinoma of the Head and Neck
NCT00446225	PHASE3	COMPLETED	Phase III Study (Tarceva®) vs Chemotherapy to Treat Advanced Non-Small Cell Lung Cancer in Patients With Mutations in the TK Domain of EGFR
NCT00448240	PHASE2/PHASE3	TERMINATED	Erlotinib (Tarceva) During First Line Standard Platinum Containing Chemo for Advanced Squamous Cell Head and Neck Cancer
NCT00457392	PHASE3	COMPLETED	A Study In Patients With Non-Small Cell Lung Cancer To Test If Erlotinib Plus SU011248 Is Better Than Erlotinib Alone
NCT00556322	PHASE3	COMPLETED	A Study of Tarceva (Erlotinib) and Standard of Care Chemotherapy in Patients With Advanced, Recurrent, or Metastatic Non-Small Cell Lung Cancer (NSCLC)
NCT00556712	PHASE3	COMPLETED	A Study of Tarceva (Erlotinib) Following Platinum-Based Chemotherapy in Patients With Advanced, Recurrent, or Metastatic Non-Small Cell Lung Cancer (NSCLC)
NCT00598156	PHASE3	COMPLETED	Chemotherapy and Avastin Followed by Maintenance Treatment With Avastin +/- Tarceva
NCT00637910	PHASE3	UNKNOWN	Tarceva Italian Lung Optimization tRial
NCT00673049	PHASE3	TERMINATED	Trial Of CP-751, 871 And Erlotinib In Refractory Lung Cancer
NCT00686114	PHASE3	UNKNOWN	Concurrent Chemoradiotherapy Containing Paclitaxel&Cisplatin With/Without Tarceva in Locally Advanced Esophageal Cancer
NCT00718315	PHASE3	COMPLETED	A Study of Verutex (Fusidic Acid), Eritex (Erythromycin) and Fisiogel in the Management of Tarceva-Associated Rash.
NCT00874419	PHASE3	COMPLETED	Erlotinib Versus Gemcitabine/Carboplatin in Chemo-naive Stage IIIB/IV Non-Small Cell Lung Cancer Patients With Epidermal Growth Factor Receptor (EGFR) Exon 19 or 21 Mutation
NCT00883779	PHASE3	COMPLETED	A Study of Tarceva (Erlotinib) or Placebo in Combination With Platinum-Based Therapy as First Line Treatment in Patients With Advanced or Recurrent Non-Small Cell Lung Cancer

Clinical evidence (CIViC)

Variant × indication × effect (209 predictive associations from 264 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib	CIViC A	EID2994 +5
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib	CIViC A	EID2995 +1
EGFR L858R OR EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Ramucirumab	CIViC A	EID11240
EGFR T790M	Lung Non-small Cell Carcinoma	Resistance	Erlotinib	CIViC A	EID238 +3
EGFR A763_Y764insFQEA	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib	CIViC B	EID5939 +3
EGFR Amplification	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID5924 +2
EGFR Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib	CIViC B	EID3794 +2
EGFR G719A	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib	CIViC B	EID4195 +1
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID229 +1
EGFR L858R	Lung Adenocarcinoma	Sensitivity/Response	Erlotinib	CIViC B	EID4290 +1
EGFR Overexpression	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib	CIViC B	EID5827 +1
BRAF V600E	Colorectal Cancer	Sensitivity/Response	Erlotinib + Vemurafenib	CIViC B	EID11427
EGFR Amplification	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib	CIViC B	EID7802
EGFR Exon 18 Overexpression	Lung Non-small Cell Carcinoma	Sensitivity/Response	Bevacizumab + Erlotinib	CIViC B	EID898
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Afatinib + Erlotinib	CIViC B	EID12202
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID413
EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Dacomitinib	CIViC B	EID4859
EGFR G719	Lung Adenocarcinoma	Sensitivity/Response	Erlotinib	CIViC B	EID1780
EGFR G719	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID4189
EGFR G719S	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID1736
EGFR L858R	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib + Afatinib	CIViC B	EID12203
EGFR L858R OR EGFR Exon 19 Deletion	Lung Adenocarcinoma	Sensitivity/Response	Erlotinib	CIViC B	EID3791
EGFR L858R OR EGFR Exon 19 Deletion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID4759
EGFR L861	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID4298
EGFR Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID2053
EGFR Mutation	Lung Cancer	Sensitivity/Response	Erlotinib	CIViC B	EID3864
EGFR Rare Exon 18-21 Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID4755
EGFR Rare Exon 18-21 Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID4762
EGFR VIII	Glioblastoma	Sensitivity/Response	Erlotinib + Gefitinib	CIViC B	EID1128
EGFR Y1092 PHOSPHORYLATION	Lung Non-small Cell Carcinoma	Sensitivity/Response	Gefitinib + Erlotinib	CIViC B	EID923

+179 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 5 clinical and 52 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

315 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Chlorpromazine	ChEMBL + PubChem	Phase 4 (approved)	EGFR, SLCO2B1
Clotrimazole	ChEMBL + PubChem	Phase 4 (approved)	EGFR, SLCO2B1
Mitoxantrone	ChEMBL + PubChem	Phase 4 (approved)	EGFR, SLCO2B1
Nelfinavir	ChEMBL + PubChem	Phase 4 (approved)	EGFR, SLCO2B1
Tamoxifen	ChEMBL + PubChem	Phase 4 (approved)	EGFR, SLCO2B1
Thioridazine	ChEMBL + PubChem	Phase 4 (approved)	EGFR, SLCO2B1
Candesartan	ChEMBL + PubChem	Phase 3 (approved)	EGFR, SLCO2B1
QUERCETIN	ChEMBL + PubChem	Phase 3 (approved)	EGFR, SLCO2B1
GENISTEIN	ChEMBL + PubChem	Phase 2 (approved)	EGFR, SLCO2B1
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR
ATAZANAVIR	ChEMBL + PubChem	Phase 4 (approved)	SLCO2B1
CYCLOSPORINE	ChEMBL + PubChem	Phase 4 (approved)	SLCO2B1
RIFAMPIN	ChEMBL + PubChem	Phase 4 (approved)	SLCO2B1
RIFAMYCIN	ChEMBL + PubChem	Phase 4 (approved)	SLCO2B1
RITONAVIR	ChEMBL + PubChem	Phase 4 (approved)	SLCO2B1
SELUMETINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR
ABEMACICLIB	ChEMBL	Phase 4 (approved)	EGFR
ACALABRUTINIB	ChEMBL	Phase 4 (approved)	EGFR
AFATINIB DIMALEATE	ChEMBL	Phase 4 (approved)	EGFR
ALECTINIB	ChEMBL	Phase 4 (approved)	EGFR
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	EGFR
AXITINIB	ChEMBL	Phase 4 (approved)	EGFR
BACITRACIN	ChEMBL	Phase 4 (approved)	EGFR
BITHIONOL	ChEMBL	Phase 4 (approved)	EGFR
BOSUTINIB	ChEMBL	Phase 4 (approved)	EGFR
BRIGATINIB	ChEMBL	Phase 4 (approved)	EGFR
CABOZANTINIB	ChEMBL	Phase 4 (approved)	EGFR
CERITINIB	ChEMBL	Phase 4 (approved)	EGFR
CHROMIC CHLORIDE	ChEMBL	Phase 4 (approved)	EGFR
CISPLATIN	ChEMBL	Phase 4 (approved)	EGFR
COLISTIN	ChEMBL	Phase 4 (approved)	EGFR
CRIZOTINIB	ChEMBL	Phase 4 (approved)	EGFR
DACOMITINIB	ChEMBL	Phase 4 (approved)	EGFR
DASATINIB	ChEMBL	Phase 4 (approved)	EGFR
DOBUTAMINE	ChEMBL	Phase 4 (approved)	EGFR
DOCETAXEL	ChEMBL	Phase 4 (approved)	EGFR
EBASTINE	ChEMBL	Phase 4 (approved)	EGFR
ECONAZOLE	ChEMBL	Phase 4 (approved)	EGFR
ELTROMBOPAG	ChEMBL	Phase 4 (approved)	SLCO2B1
FEDRATINIB	ChEMBL	Phase 4 (approved)	EGFR
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	EGFR
GEFITINIB	ChEMBL	Phase 4 (approved)	EGFR
GENTIAN VIOLET	ChEMBL	Phase 4 (approved)	EGFR
GILTERITINIB	ChEMBL	Phase 4 (approved)	EGFR
HEXACHLOROPHENE	ChEMBL	Phase 4 (approved)	EGFR
IBRUTINIB	ChEMBL	Phase 4 (approved)	EGFR
IMATINIB	ChEMBL	Phase 4 (approved)	EGFR
LAPATINIB	ChEMBL	Phase 4 (approved)	EGFR
LAPATINIB DITOSYLATE	ChEMBL	Phase 4 (approved)	EGFR
LAZERTINIB	ChEMBL	Phase 4 (approved)	EGFR
LEVODOPA	ChEMBL	Phase 4 (approved)	EGFR
LORLATINIB	ChEMBL	Phase 4 (approved)	EGFR
METHYLDOPA	ChEMBL	Phase 4 (approved)	EGFR
MICONAZOLE	ChEMBL	Phase 4 (approved)	EGFR
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	EGFR
MOBOCERTINIB	ChEMBL	Phase 4 (approved)	EGFR
MONTELUKAST	ChEMBL	Phase 4 (approved)	EGFR
NERATINIB	ChEMBL	Phase 4 (approved)	EGFR
NICLOSAMIDE	ChEMBL	Phase 4 (approved)	EGFR
OLMUTINIB	ChEMBL	Phase 4 (approved)	EGFR